Mesterolone (Proviron) has androgenic properties. Early studies suggested oral
mesterolone did not usually suppress gonadotrophins or endogenous
testosterone production. A later single dose study suggests there may be a
central suppression effect at doses of 75-100 mg daily.

Following oral ingestion mesterolone is rapidly absorbed. In a study in 18 men
the intake of Proviron 25 mg generated maximum serum drug levels of 3.1 ± 1.1
ng/mL after 1.6 ± 0.6 hours. Thereafter, drug levels in serum decrease with a
terminal half-life of 12 - 13 hours. Mesterolone is bound to serum proteins by 98
%. Binding to albumin accounts for 40 % and binding to SHBG (sex hormone
binding globulin) to 58 %.
Mesterolone is rapidly metabolised. The metabolic clearance rate from serum
accounts for 4.4 ± 1.6 mL·min-1·kg-1. Renal excretion of unchanged drug has not
been detected. In a study of C14 labelled mesterolone in two men, up to 2% of
mesterolone was excreted as the conjugated form in the urine. The main
metabolite has been identified as 1α-methyl-androsterone, which - in conjugated
form - accounts for 55 - 70 % of renally excreted metabolites. The ratio of
conjugated main metabolite glucuronide to sulfate detected in urine was about
12:1. As a further metabolite 1α-methyl-5α-androstane-3α,17β-diol has been
recognized, which accounted for about 3 % of renally eliminated metabolites.
Mesterolone was excreted in the form of metabolites. Within 7 days
approximately 80% of the labelled doses were recovered in the urine and up to
13% in the faeces. Half of the labelled doses were excreted in the urine within 24
hours.
The absolute bioavailability of mesterolone was determined to be about 3 % of
the oral dose.

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